Synthesis, biological evaluation and in silico and in vitro mode-of-action analysis of novel dihydropyrimidones targeting PPAR-gamma

Hepatocellular carcinoma, a fatal liver cancer, affects 600 000 people annually and ranks third in cancer-related lethality. In this work we report the synthesis and related biological activity of novel dihydropyrimidones. Among the tested compounds, 5-acetyl-4-(1H-indol- 3-yl)-6-methyl-3,4-dihydropyrimidin-2(1H)-one (4g) was found to be most active towards the HepG2 cell line (IC50 = 17.9 mu M), being at the same time 7.6-fold selective over normal (LO2) liver cells (IC50 = 136.9 mu M). Subsequently, we identified peroxisome proliferator-activated receptor gamma as a target of compound 4g using an in silico approach, and confirmed this mode-of-action experimentally

Evaluation of the sensitivity of electro-acousic measurements for process monitoring and control of an atmospheric pressure plasma jet system

The development of non-invasive process diagnostic techniques for the control of atmospheric plasmas is a critical issue for the wider adoption of this technology. This paper evaluates the use of a frequency-domain deconvolution of an electro-acoustic emission as a means to monitor and control the plasma formed using an atmospheric pressure plasma jet (APPJ) system. The air plasma system investigated was formed using a PlasmaTreat™ OpenAir applicator. Change in the electro-acoustic signal with changes in substrate type (ceramic, steel, polymer). APPJ nozzle to substrate distance and substrate feature size were monitored. The decoding of the electro-acoustic emission yields three sub dataset that are described three separate emission mechanisms. The three emissions are associated with: the power supply fundamental drive frequency and its harmonics; the APPJ nozzle longitudinal mode acoustic emission and its odd overtones, and the acoustic surface reflection that is produced by the impedance mismatch between the discharge and the surface. Incorporating this knowledge into a LabVIEW a program facilitated the continuous deconvolution of the electro-acoustic data. This enabled the use of specific frequency band test limits to control the process the APPJ treatment process which is sensitive to both plasma processing conditions and substrate type and features. PAC Codes: 52.40.Hf, 52.70.-m, 52.77.Fv, 43.60.VxScience Foundation IrelandAuthor has checked copyrightAD 22/01/201